Cathepsin Inhibitor 1 ≥99%

(S)-3-(tert-butyl)-N-(3-(3-chlorophenyl)-1-((cyanomethyl)amino)-1-oxopropan-2-yl)-1-methyl-1H-pyrazole-5-carboxamide

源叶(MedMol)
Y31549
225120-65-0
C20H24ClN5O2
401.89
Cathepsin Inhibitor 1; Cathepsin-Inhibitor-1; CTS-IN-1; CTS IN 1;组织蛋白酶抑制剂1
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) Y31549-1mg ≥99% ¥335.00元 10 - - -
源叶(MedMol) Y31549-5mg ≥99% ¥765.00元 6 - - -
源叶(MedMol) Y31549-10mg ≥99% ¥1275.00元 6 - - -
源叶(MedMol) Y31549-25mg ≥99% ¥2380.00元 6 - - -
源叶(MedMol) Y31549-100mg ≥99% ¥6800.00元 预计交期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
产品描述: Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
靶点: Cathepsin L2:6.7(pIC50), Cathepsin B:5.2(pIC50), Cathepsin S:6(pIC50), cathepsin K:5.5(pIC50), Cathepsin L:7.9(pIC50);CysteineProtease
体外研究: The CatL pIC50 value of Cathepsin Inhibitor 1 was found to exceed that of its analog by 1.6 units. Moreover, CatS (ΔpIC50 = -0.1) and CatL2 (ΔpIC50 = 0.5) were much less sensitive to the structural change of Cathepsin Inhibitor 1, leading to an improved selectivity profile relative to its analog. Cathepsin Inhibitor 1 was as least as selective with respect to CatB and CatS as previously described CatL inhibitors. The crystal structure of its another analog bound to CatL provided the rationale for the SAR observed for Cathepsin Inhibitor 1. The 1-methyl group of the pyrazole made some contact with Leu69 and appeared to force the pyrazole ring out of co-planarity with the amide, likely functioning as a conformational lock
体内研究: Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats.
参考文献: 1. Asaad N, et al. Dipeptidyl nitrile inhibitors of Cathepsin L. Bioorg Med Chem Lett, 2009, 19(15), 4280-4283.
溶解性: Soluble  in  DMSO、Ethanol
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.488 ml 12.441 ml 24.882 ml
5 mM 0.498 ml 2.488 ml 4.976 ml
10 mM 0.249 ml 1.244 ml 2.488 ml
50 mM 0.05 ml 0.249 ml 0.498 ml
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参考文献

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